[STUDY OF THE CYTOTOXIC ACTIVITY OF INDOLE ALKALOIDS FROM THE ABOVEGROUND ORGANS OF VINCA ROSEA L. INTRODUCED IN WESTERN GEORGIA].

The objects of this research were the aboveground and underground parts of Vinca rosea L., a species of periwinkle introduced in Western Georgia. The sum of alkaloids and biologically aactive fractions of monomeric alkaloids were obtained by liquid-liquid extraction, precipitation with petroleum ether (I), polybuffer distribution (II) and 10% acetic acid (III). 14 known compounds were identified by LC-MS/MS and GC/MS: Low molecular weight compounds (М+226, М+202, №1,2, М+168) and alkaloids Ajmalicine, Tetragidroalstonine, C20-dihydrova llesiahotamine, C19-C20 Vallesiahotaminole, Vallesiahotamine lacton, Polyneuridine, Pericy clivine, Lochnerame, Norharmane, Vidorosine, Vindolinine, Isovindolinine, Akuammicine. The cytotoxicity of monomeric alkaloids was evaluated for A-549 (cells of the lung cancer line), DLD-1 (cells of the rectal adenocarcinoma line) and W-1 (cells of the normal human fibroblast line). All three substances (I, II, III) showed pronounced cytotoxic activity.

[BIOLOGICALLY ACTIVE ALKALOIDS FROM RHIZOMES WITH ROOTS OF VINCA HERBACEA WALDST. ET KIT, GROWING IN GEORGIA].

Roots and rhizomes of Vinca herbacea Waldst. et Kit, were collected during early flowering and fruiting. Рhenophases biologically active substances I and II were obtained by liquid-liquid extraction. Dominant alkaloids: tabersonin, reserpine, maidine, norfluorocurarin and copsinin were obtained after the dispertion in citrare-phosfhate buffer and subsequent TLC. Accelerated restitution of granulocytopoiesis was observed in mice during both irradiation and myelotoxic drug-induced acute leucopenia. Increase in total WBC over 200% was observed after treatment by substance I in drug-induced leucopenia model (fivefold oral administration) and over 130% after treatment by substance I in irradiate mice (fivefold intraperitoneal administration). Morphological and anatomical structures of the underground organs of V. herbacea have been studied. The main microstructural characteristics are revealed - Rhizomes are characterized by coutinized epidermis, lamellar collenchyma, fibers and the texture of the vascular system of a monocyclic structure. The root system shows the whole cortex, the endoderm with Kaspar spots; the outer, radially continuous phloem tissue is located in the conducting system and distinguishes the cylindrical xylem tissue with annular and spiral-circular blood vessels.

[SCREENING OF WILD SPREAD AND CULTIVATED OF BUXUS SPECIES GROWING IN GEORGIA ON THE CONTENT OF ALKALOIDS AND BIOLOGICAL ACTIVITY].

Georgian flora is represented by about 4150 plant species. Many important alkaloid-containing plant species and among of them are species Buxus L. of genus in Adjara. The aims of the research were: sequential screening of the plants for the consistence of alkaloids; Study of anatomical characteristics of Buxus colchica Pojark. and revealing of specific pharmacological activity of steroidal alkaloids. The objects of research were B. colchica, B. balearika and B. sempervirens, growing in Adjara (Georgia), collected in active phase of flowering of the plants. There were revealed 370 species of alkaloid containing plants. Sum of alkaloids and crude aqueous extract have spasmolitic and antihistaminic activity. Experimental anatomical research of diagnostic characteristics of the bines showed the existence of monocyclic transient system with fiber like tracheids, dorsoventral mesophyll of the leaves; the structure for the upper part of epidermis is linear and the lower part is curved, type of stomata is paracitic.

[ALKALOIDS OF PEGANUM HARMALA L. AND THEIR BIOLOGICAL ACTIVITY].

Peganum Harmala L., Peganасеае widely distributed in Georgia. On the basis of chemical analysis of the composition of alkaloids it was found out that the plant contains quinazoline derivatives, among which dominats alkaloid d, 1 peganine: С11Н12NО2, m.p. 198-99ºC (СН3ОН). UV, λmax 275 (lgε 3,95). In IR-spectrum (KBr) 1625 cm- (-N=C) 3200-370 (OH)cm-1 . Mass- spectrum: М+ 171(100%). It was studied the dynamics of accumulation for total alkaloids and d, l - peganine: in the budding phase the amount of alkaloids was - 3,71%, d, l - peganine 0,07÷0,09%; in the phase of mass flowering the sum of alkaloids - 4,51% ,d, l - peganine - 0,1÷0,13%; in the phase of ripeness total alkaloids - 3.92%; d,l - peganine - 0,08÷0,1. The study of specific pharmacological activity showed that the d,l - peganine similar to peganine at a dose of 30 mg/kg causes a decrease in heart rate by 30÷40 beats/min, which is characteristic for anticholinesterases, in parallel with this, a decrease in cholinesterase activity in blood serum has been observed.

[Analysis of some species of magnolia introduced to west georgia, on content of aporphine alkaloids and their biological activity].

The goal of research was study of vegetative organs of Magnolia species introduced to west Georgia on qualitative and quantitative content of aporphine alkaloids and evaluate cytotoxic activity of total alkaloids from M. officinalis and M. glauca against A-549, DLD-1 and WS-1. Qualitative and quantitative content of aporphine alkaloids in different vegetative organs were determined by chromatographic methods. Based on the researches alkaloids - liriodenine and lanuginozine are characteristic for leaves, for bark of branches - liriodenine, d-caaverine; for bark of trunk - a liriodenine, a caaverine and a magnoflorine. Liriodenine may be considered as is chemotaxonomic sign of genus Magnolia, as it was found in all analyzed vegetative organs. In vitro cytotoxic activity of total alkaloids of M. officinalis and M. glauca has been investigated against DLD-1, WS-1 and A-549. Total alkaloids of M. glauca expressed significant cytotoxic activity against DLD-1 and WS-1, and medium cytotoxicity against A-549; M. officinalis exerted middle activity against A-549, DLD-1, WS-1.

[Alkaloids of Vinca rosea L. introduced to Western Georgia].

Vinca roseae L. (Саtharanthus rosea (L.) G. Don) was introduced at Kobuleti experimental station of medical plants. The object of investigation was the plant material of Vinca roseae L. collected in May, 2005., September, 2006 and October, 2009. Total alkaloids were obtained in accordance with Atta- ur-Rachman method. The variability of the quantitative and qualitative composition of total alkaloids and vincaleikoblastin (VLB) fraction during vegetation was studied. It was established that the maximal content of total alkaloids and VLB fraction of Vinca roseae L. is accumulated in the phase of secondary flowering, hence the collecting of a plant material is recommended to be made during the aforesaid vegetation phase as for this period it is a rather high output of a raw material, alkaloid complex and VLB faction. Alkaloids vinkaleikoblastin, ajmalicine and new epimer tetrahydroalstonine with С3Н-α- orientation were yielded, separated and identified using modern physical-chemical and spectral methods (13С NMR).

[Extraction of pharmacologically active alkaloids from Vinca species].

From the Genius Vinca the drugs have been received, arbitrally named: Vingerbin- with anthyarithmic activity, Vincabral-for improvement of brain blood circulation and leicobetin-as stimulator of leicopoesis. The investigations has been performed for creation of rational, resource saving, rentable phyto technologies. As a result, the liquid extraction general schema is provided for receipt of indolic alkaloids from plants V. herbaceae and V.minor. Analyses have shown that extraction with diluent gaz gives the possibility to receive the sums rich with alkaloids:Vingerbin and Vincabral. The advantage of extraction with diluent gaz is exclusion of high volumes of organic and non organic chemicals on the stage of extraction from raw material and liquid extraction, and remain and lipofil fraction converse to new phytosubtances for receipt of biologically active flavonoids, amino acids etc.